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Assay Detail

CHEMBL1953151

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptor
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3372)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.
Tripathy R, McHugh RJ, Bacon ER, Salvino JM, Morton GC, Aimone LD, Huang Z, Mathiasen JR, DiCamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Qian J, Angeles TS, Connors T, Spais C, Holskin B, Duzic E, Schaffhauser H, Rossé GC.
Bioorg Med Chem Lett (2012) 22 : 1421 -1426
PubMed 22226656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.87 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1949930 2 7.57
CHEMBL1949764 1 7.40
CHEMBL1949763 1 7.28
CHEMBL1949762 1 6.87
CHEMBL1949760 1 6.84
CHEMBL1949768 1 6.81
CHEMBL1949773 2 6.76
CHEMBL1949761 1 6.69
CHEMBL1949772 1 6.63
CHEMBL1949765 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1949930 Ki = 27.0 nM 7.57
CHEMBL1949764 Ki = 40.0 nM 7.40
CHEMBL1949763 Ki = 52.0 nM 7.28
CHEMBL1949930 Ki = 55.0 nM 7.26
CHEMBL1949762 Ki = 136.0 nM 6.87
CHEMBL1949760 Ki = 145.0 nM 6.84
CHEMBL1949768 Ki = 156.0 nM 6.81
CHEMBL1949773 Ki = 174.0 nM 6.76
CHEMBL1949761 Ki = 206.0 nM 6.69
CHEMBL1949772 Ki = 236.0 nM 6.63
CHEMBL1949765 Ki = 243.0 nM 6.61
CHEMBL1949773 Ki = 2181.0 nM 5.66